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5FTO
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CRYSTAL STRUCTURE OF THE ALK KINASE DOMAIN IN COMPLEX WITH ENTRECTINIB
分子名称:ALK TYROSINE KINASE RECEPTOR, Entrectinib
著者Bossi, R., Canevari, G., Fasolini, M., Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Buffa, L., Ceriani, L., Colombo, M., Corti, L., Donati, D., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Lombardi Borgia, A., Marchionni, C., Nesi, M., Orrenius, C., Panzeri, A., Perrone, E., Pesenti, E., Rusconi, L., Saccardo, M.B., Vanotti, E., Orsini, P.
登録日2016-01-14
公開日2016-04-06
最終更新日2016-04-27
実験手法X-RAY DIFFRACTION (2.22 Å)
主引用文献Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (Alk), C-Ros Oncogene 1 Kinase (Ros1), and Pan-Tropomyosin Receptor Kinases (Pan-Trks) Inhibitor.
J.Med.Chem., 59, 2016
5FTQ
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CRYSTAL STRUCTURE OF THE ALK KINASE DOMAIN IN COMPLEX WITH CMPD 17
分子名称:ALK TYROSINE KINASE RECEPTOR, N-[5-(3,5-DIFLUOROBENZYL)-1H-INDAZOL-3-YL]-2-[(4-HYDROXYCYCLOHEXYL)AMINO]-4-(4-METHYLPIPERAZIN-1-YL) BENZAMIDE, GLYCEROL
著者Bossi, R., Canevari, G., Fasolini, M., Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Buffa, L., Ceriani, L., Colombo, M., Corti, L., Donati, D., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Lombardi Borgia, A., Marchionni, C., Nesi, M., Orrenius, C., Panzeri, A., Perrone, E., Pesenti, E., Rusconi, L., Saccardo, M.B., Vanotti, E., Orsini, P.
登録日2016-01-14
公開日2016-04-06
最終更新日2016-04-27
実験手法X-RAY DIFFRACTION (1.7 Å)
主引用文献Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (Alk), C-Ros Oncogene 1 Kinase (Ros1), and Pan-Tropomyosin Receptor Kinases (Pan-Trks) Inhibitor.
J.Med.Chem., 59, 2016
1R0P
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET IN COMPLEX WITH THE MICROBIAL ALKALOID K-252A
分子名称:Hepatocyte growth factor receptor, K-252A
著者Schiering, N., Knapp, S., Marconi, M., Flocco, M.M., Cui, J., Perego, R., Rusconi, L., Cristiani, C.
登録日2003-09-22
公開日2003-10-07
最終更新日2017-10-11
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a
Proc.Natl.Acad.Sci.USA, 100, 2003
1R1W
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CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET
分子名称:HEPATOCYTE GROWTH FACTOR RECEPTOR
著者Schiering, N., Knapp, S., Marconi, M., Flocco, M.M., Cui, J., Perego, R., Rusconi, L., Cristiani, C.
登録日2003-09-25
公開日2003-10-07
最終更新日2017-10-11
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a
Proc.Natl.Acad.Sci.USA, 100, 2003
2JGB
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STRUCTURE OF HUMAN EIF4E HOMOLOGOUS PROTEIN 4EHP WITH M7GTP
分子名称:EUKARYOTIC TRANSLATION INITIATION FACTOR 4E TYPE 2, EUKARYOTIC TRANSLATION INITIATION FACTOR 4E-BINDING PROTEIN 1, 7N-METHYL-8-HYDROGUANOSINE-5'-TRIPHOSPHATE
著者Cameron, A.D., Rosettani, P., Knapp, S., Vismara, M.G., Rusconi, L.
登録日2007-02-12
公開日2007-02-27
最終更新日2018-03-28
実験手法X-RAY DIFFRACTION (1.7 Å)
主引用文献Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms.
J. Mol. Biol., 368, 2007
2JGC
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STRUCTURE OF THE HUMAN EIF4E HOMOLOGOUS PROTEIN, 4EHP WITHOUT LIGAND BOUND
分子名称:EUKARYOTIC TRANSLATION INITIATION FACTOR 4E TYPE 2, EUKARYOTIC TRANSLATION INITIATION FACTOR 4E-BINDING PROTEIN 1
著者Cameron, A.D., Rosettani, P., Knapp, S., Vismara, M.G., Rusconi, L.
登録日2007-02-12
公開日2007-02-27
最終更新日2018-03-28
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms.
J. Mol. Biol., 368, 2007
2V7A
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CRYSTAL STRUCTURE OF THE T315I ABL MUTANT IN COMPLEX WITH THE INHIBITOR PHA-739358
分子名称:PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1, N-[(3E)-5-[(2R)-2-METHOXY-2-PHENYLACETYL]PYRROLO[3,4-C]PYRAZOL-3(5H)-YLIDENE]-4-(4-METHYLPIPERAZIN-1-YL)BENZAMIDE, MAGNESIUM ION
著者Modugno, M., Casale, E., Soncini, C., Rosettani, P., Colombo, R., Lupi, R., Rusconi, L., Fancelli, D., Carpinelli, P., Cameron, A.D., Isacchi, A., Moll, J.
登録日2007-07-27
公開日2007-09-18
最終更新日2019-10-16
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Crystal Structure of the T315I Abl Mutant in Complex with the Aurora Kinases Inhibitor Pha-739358.
Cancer Res., 67, 2007
2X9E
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HUMAN MPS1 IN COMPLEX WITH NMS-P715
分子名称:DUAL SPECIFICITY PROTEIN KINASE TTK, N-(2,6-DIETHYLPHENYL)-1-METHYL-8-({4-[(1-METHYLPIPERIDIN-4-YL)CARBAMOYL]-2-(TRIFLUOROMETHOXY)PHENYL}AMINO)-4,5-DIHYDRO-1H-PYRAZOLO[4,3-H]QUINAZOLINE-3-CARBOXAMIDE
著者Colombo, R., Caldarelli, M., Mennecozzi, M., Giorgini, M.L., Sola, F., Cappella, P., Perrera, C., DePaolini, S.R., Rusconi, L., Cucchi, U., Avanzi, N., Bertrand, J.A., Bossi, R.T., Pesenti, E., Galvani, A., Isacchi, A., Colotta, F., Donati, D., Moll, J.
登録日2010-03-17
公開日2010-12-29
最終更新日2019-03-27
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献Targeting the Mitotic Checkpoint for Cancer Therapy with Nms-P715, an Inhibitor of Mps1 Kinase.
Cancer Res., 70, 2010
2XB7
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STRUCTURE OF HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH NVP- TAE684
分子名称:ALK TYROSINE KINASE RECEPTOR, 5-CHLORO-N-[2-METHOXY-4-[4-(4-METHYLPIPERAZIN-1-YL)PIPERIDIN-1-YL]PHENYL]-N'-(2-PROPAN-2-YLSULFONYLPHENYL)PYRIMIDINE-2,4-DIAMINE
著者Bossi, R.T., Saccardo, M.B., Ardini, E., Menichincheri, M., Rusconi, L., Magnaghi, P., Orsini, P., Fogliatto, G., Bertrand, J.A.
登録日2010-04-08
公開日2010-07-28
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Crystal Structures of Anaplastic Lymphoma Kinase in Complex with ATP Competitive Inhibitors.
Biochemistry, 49, 2010
2XBA
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STRUCTURE OF HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH PHA- E429
分子名称:ALK TYROSINE KINASE RECEPTOR, 5-[(2R)-2-hydroxy-2-phenylacetyl]-3-({[4-(4-methylpiperazin-1-yl)phenyl]carbonyl}amino)-1,6-dihydropyrrolo[3,4-c]pyrazol-5-ium
著者Bossi, R.T., Saccardo, M.B., Ardini, E., Menichincheri, M., Rusconi, L., Magnaghi, P., Orsini, P., Fogliatto, G., Bertrand, J.A.
登録日2010-04-08
公開日2010-07-28
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Crystal Structures of Anaplastic Lymphoma Kinase in Complex with ATP Competitive Inhibitors.
Biochemistry, 49, 2010
2BMC
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AURORA-2 T287D T288D COMPLEXED WITH PHA-680632
分子名称:SERINE THREONINE-PROTEIN KINASE 6, (3E)-N-(2,6-DIETHYLPHENYL)-3-{[4-(4-METHYLPIPERAZIN-1-YL)BENZOYL]IMINO}PYRROLO[3,4-C]PYRAZOLE-5(3H)-CARBOXAMIDE
著者Cameron, A.D., Izzo, G., Sagliano, A., Rusconi, L., Storici, P., Fancelli, D., Berta, D., Bindi, S., Catana, C., Forte, B., Giordano, P., Mantegani, S., Meroni, M., Moll, J., Pittala, V., Severino, D., Tonani, R., Varasi, M., Vulpetti, A., Vianello, P.
登録日2005-03-11
公開日2005-03-17
最終更新日2019-08-21
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Potent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition.
J.Med.Chem., 48, 2005
2IVX
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CRYSTAL STRUCTURE OF HUMAN CYCLIN T2 AT 1.8 A RESOLUTION
分子名称:CYCLIN-T2, 1,2-ETHANEDIOL
著者Debreczeni, J.E., Bullock, A.N., Fedorov, O., Savitsky, P., Berridge, G., Das, S., Pike, A.C.W., Turnbull, A., Ugochukwu, E., Papagrigoriou, E., Gorrec, F., Sundstrom, M., Edwards, A., Arrowsmith, C., Weigelt, J., von Delft, F., Knapp, S.
登録日2006-06-21
公開日2006-07-19
最終更新日2019-05-08
実験手法X-RAY DIFFRACTION (1.8 Å)
主引用文献The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation.
EMBO J., 27, 2008
2J4Z
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STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626
分子名称:SERINE THREONINE-PROTEIN KINASE 6, 4-(4-METHYLPIPERAZIN-1-YL)-N-[5-(2-THIENYLACETYL)-1,5-DIHYDROPYRROLO[3,4-C]PYRAZOL-3-YL]BENZAMIDE, ARSENIC
著者Cameron, A.D., Izzo, G., Storici, P., Rusconi, L., Fancelli, D., Varasi, M., Berta, D., Bindi, S., Forte, B., Severino, D., Tonani, R., Vianello, P.
登録日2006-09-08
公開日2006-11-06
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.
J. Med. Chem., 49, 2006
2J50
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STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-739358
分子名称:SERINE/THREONINE-PROTEIN KINASE 6, N-[(3E)-5-[(2R)-2-METHOXY-2-PHENYLACETYL]PYRROLO[3,4-C]PYRAZOL-3(5H)-YLIDENE]-4-(4-METHYLPIPERAZIN-1-YL)BENZAMIDE, SULFATE ION
著者Cameron, A.D., Izzo, G., Storici, P., Rusconi, L., Fancelli, D., Varasi, M., Berta, D., Bindi, S., Forte, B., Severino, D., Tonani, R., Vianello, P.
登録日2006-09-08
公開日2006-11-06
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile.
J.Med.Chem., 49, 2006
3BLH
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CRYSTAL STRUCTURE OF HUMAN CDK9/CYCLINT1
分子名称:Cell division protein kinase 9, Cyclin-T1, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL
著者Baumli, S., Lolli, G., Lowe, E.D., Johnson, L.N.
登録日2007-12-11
公開日2008-07-01
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation
Embo J., 27, 2008
3BLQ
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CRYSTAL STRUCTURE OF HUMAN CDK9/CYCLINT1 IN COMPLEX WITH ATP
分子名称:Cell division protein kinase 9, Cyclin-T1, MAGNESIUM ION, ...
著者Baumli, S., Lolli, G., Lowe, E.D., Johnson, L.N.
登録日2007-12-11
公開日2008-07-01
最終更新日2017-10-25
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation
Embo J., 27, 2008
3BLR
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CRYSTAL STRUCTURE OF HUMAN CDK9/CYCLINT1 IN COMPLEX WITH FLAVOPIRIDOL
分子名称:Cell division protein kinase 9, Cyclin-T1, PHOSPHATE ION, ...
著者Baumli, S., Lolli, G., Lowe, E.D., Johnson, L.N.
登録日2007-12-11
公開日2008-07-01
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation
Embo J., 27, 2008